| Literature DB >> 12372843 |
J J Kopchick1, C Parkinson, E C Stevens, P J Trainer.
Abstract
An understanding of the events that occur during GH receptor (GHR) signaling has facilitated the development of a GHR antagonist (pegvisomant) for use in humans. This molecule has been designed to compete with native GH for the GHR and to prevent its proper or functional dimerization-a process that is critical for GH signal transduction and IGF-I synthesis and secretion. Clinical trials in patients with acromegaly show GHR blockade to be an exciting new mode of therapy for this condition, and pegvisomant may have a therapeutic role in diseases, such as diabetes and malignancy, in which abnormalities of the GH/IGF-I axis have been observed. This review charts the discovery and development of GHR antagonists and details the experience gained in patients with acromegaly.Entities:
Mesh：
Substances：
Year: 2002 PMID： 12372843 DOI： 10.1210/er.2001-0022
Source DB: PubMed Journal: Endocr Rev ISSN： 0163-769X Impact factor: 19.871